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Pharmacokinetic comparison between quercetin and quercetin 3-O-?-glucuronide in rats by UHPLC-MS/MS.

ABSTRACT: Quercetin is a natural flavonoid widely distributed in human diet and functional foods. Quercetin 3-O-?-glucuronide (Q3G) is present in wine and some medicinal plants. Quercetin and Q3G may be metabolized from each other in vivo. While quercetin has been the subject of many studies, the pharmacokinetic profiles of quercetin and Q3G (in animals) have not yet been compared. Herein, we prepared a column-based method for rapid isolation of Q3G from Nelumbo nucifera. Then, we developed an UHPLC-MS/MS method to compare the pharmacokinetics of quercetin and Q3G. Our results showed that the plasma concentration-time curves of quercetin and Q3G show two maxima (T_max1???0.75?h, T_max2???5?h). After oral administration of 100?mg/kg quercetin or 100?mg/kg Q3G in rats, predominantly Q3G was detected in plasma with AUC at 39529.2?±?6108.2?mg·h·L^-1 or 24625.1?±?1563.8?mg·h·L^-1, 18-fold higher than quercetin with AUC at 1583.9?±?583.3?mg·h·L^-1 or 1394.6?±?868.1?mg·h·L^-1, respectively. After intravenous injection of 10?mg/kg in rats, Q3G showed extensive tissue uptake in kidney (409.2?±?118.4?ng/g), liver (166.1?±?52.9?ng/g), heart (97.7?±?22.6?ng/g), and brain (5.8?±?1.2?ng/g). In conclusion, we have shown that Q3G is a major active component in plasma and tissue for oral administration of quercetin or Q3G.

SUBMITTER: Yang LL

PROVIDER: S-EPMC5075792 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:An accurate and precise liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS) method was developed and validated for the pharmacokinetic study of epiprogoitrin and progoitrin, a pair of epimers that can be deglycosylated to epigoitrin and goitrin, respectively. These analytes were administered intravenously or intragastrically to male Sprague-Dawley rats, and the influence of 3(R/S)-configuration on the pharmacokinetics of both epimers in rat plasma was elucidated. The analytes and an internal standard (i.e., sinigrin) were resolved by LC-MS/MS on a reverse-phase ACQUITY UPLC™ HSS T3 column equilibrated and eluted with acetonitrile and water (0.1 % formic acid) at a ?ow rate of 0.3?mL/min. Quantitation was achieved by applying the multiple reaction monitoring mode, in the negative ion mode, at transitions of m/z 388 ? 97 and m/z 358 ? 97 for the epimers and sinigrin, respectively. The method demonstrated good linearity over the concentration range of 2-5000?ng/mL (r > 0.996). The lower limit of quantification for epiprogoitrin and progoitrin was 2?ng/mL. The interday and intraday accuracy and precision were within ±15 %. The extraction recovery, stability, and matrix effect were demonstrated to be within acceptable limits. The validated method was thus successfully applied for the pharmacokinetic study of both the epimers. After the rats received the same oral dose of the epimers, the pharmacokinetic profiles were similar. The maximum plasma concentration (Cmax) and AUC values of epiprogoitrin were a bit higher than those of progoitrin, whereas the pharmacokinetic behaviours of the epimers were obviously different upon intravenous administration. The Cmax and AUC values of epiprogoitrin were approximately three-fold higher than those of progoitrin, and the half-life of progoitrin was much shorter than that of epiprogoitrin. The oral bioavailability of progoitrin was 20.1 %-34.1 %, which is three times higher than that of epiprogoitrin.

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Pharmacokinetic comparison between quercetin and quercetin 3-O-?-glucuronide in rats by UHPLC-MS/MS.

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